Kinesin Inhibitor

Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a K_{i app} of 1.7 nM.

Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC₅₀ value of 14 μM.

Sovilnesib (AMG 650) is a potent, orally active kinesin-like protein KIF18A inhibitor with an IC₅₀ value of 0.071 μM. Sovilnesib can be used for the research of cancer.

S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC₅₀ of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities.

GSK-923295 is a special, allosteric inhibitor of centromere-associated protein-E (CENP-E) kinesin motor ATPase activity, with K_i of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.

Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC₅₀ of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.

(R)-Filanesib ((R)-ARRY-520) is an isomer of Filanesib (HY-15187). Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC₅₀ of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.

Filanesib hydrochloride (ARRY-520 hydrochloride) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC₅₀ of 6 nM for human KSP. Filanesib hydrochloride induces cell death by apoptosis in vitro. Filanesib hydrochloride has potent anti-proliferative activity.

AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a K_i of 43 nM and an IC₅₀ of 300 nM for KIFC1.

Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC₅₀ of 1.35 μM and a K_i of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC₅₀ of 5.5 μM.

KIF18A-IN-6 (Compound 134) is an orally active KIF18A inhibitor with an IC₅₀ of 0.016 μM against KIF18A microtubule-dependent ATPase activity.

SB-743921 hydrochloride is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a K_i of 0.1 nM.

Dimethylenastron is a potent kinesin Eg5 inhibitor, with an IC₅₀ of 200 nM.

VLS-1272 (Compound 22) is an orally active KIF18A inhibitor that binds to the KIF18A-microtubule complex in an ATP-noncompetitive manner (IC₅₀ = 41 nM), blocking its ATPase activity and inhibiting microtubule translocation. This leads to abnormal accumulation of KIF18A at spindle poles, disrupting chromosome alignment and inducing mitotic arrest and apoptosis in CIN^High tumor cells (e.g., ovarian cancer OVCAR-3, breast cancer JIMT-1). VLS-1272 is a promising candidate for anti-tumor research.

Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member 15 (Kif15), and is used for the research of cellular proliferative diseases.

MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC₅₀ of 2.2 nM and a pK_a of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy.

CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC₅₀ of 75 μM.

BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC₅₀ of 1.69 μM.

Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.

KIF18A-IN-1 is an inhibitor of the mitotic kinesin KIF18A with anti-tumor activity. KIF18A targeted inhibitors may activate mitotic checkpoints and selectively kill chromosomally unstable cancer cells.